Formulation optimization and Evaluation of Transdermal patch of losartan potassium containing DMSO as permeation enhancer

Jadhav, Sachin; Koshti, Ankita R.; Bari, M. M.; Barhate, Shashikant D.

doi:10.5958/2231-5713.2019.00037.0

Cited by 5 publications

(3 citation statements)

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“…In addition, the presence of EA increases the permeability by fluidizing lipid bilayers [ 64 ]. Thus, drug permeability through membranes may be attributed to size, lipophilicity and deformability of transfersomes [ 28 ].…”

Section: Discussionmentioning

confidence: 99%

“…The significance of current research work is that transfersomes-loaded oral films offer more absorptive properties than existing EBT formulations. Besides, transfersomes have the ability to diffuse through lipid membranes by modulating the membrane bilayer structure, acting as a permeation enhancer and making pathway to improve the absorption of drug molecules [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

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Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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“…The area which is specified of the patch is to be cut in different parts of the patch and weigh it on a digital balance. The average weight of the all sections and standard deviation values are to be calculated from the individual weight and the weight uniformity is calculated 34 .…”

Section: Weight Uniformitymentioning

confidence: 99%

Untitled

2022

IJPSR

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Currently, oral drug delivery and parenteral drug delivery are used for the treatment of various diseases. In the oral drug delivery system, due to the first-pass metabolism and acidic environment of the gastrointestinal route, the drug exposes to acids and enzymes present in the gastrointestinal tract, which may lead to degradation of the compound, which ultimately results in poor bioavailability of the molecule. On the other hand, the parenteral drug delivery system has its own disadvantages as it is invasive and needs skilled personnel for administration. To overcome these problems, the transdermal drug delivery system is introduced as a novel approach, and recently there is tremendous interest in transdermal drug delivery systems. A transdermal patch is a medicated adhesive patch winch that is placed onto the skin to deliver the appropriate dose of the drug through the skin and directly into the bloodstream. In this, transdermal patches are prepared for drug penetration through the skin layer (Stratum corneum barrier). To avoid the stratum corneum barrier, the microneedle-based transdermal drug delivery system is advantageous. Microneedles are classified into solid microneedles, coated microneedles, dissolving microneedles, hollow microneedles, and hydrogel-forming microneedles. This review provides information regarding transdermal drug delivery, a factor that can affect the transdermal delivery, ingredients used in the formulation of TDDS, drug penetration, different types of methods for formulations, and some advanced techniques such as microneedles. INTRODUCTION:Recently, there is growing interest in the novel drug delivery system for existing drug molecules. The novel drug delivery system offers to increased safety and efficiency of a drug molecule and also improves patient compliance. Transdermal drug delivery systems (TDDS) are self-contained and discrete dosage forms. Another advantage of the TDDS is that the dose is reduced as compared to the oral route of drug delivery 1 .

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Formulation and Evaluation of Transdermal patch of Methimazole

Tadhi

Chopra

Sharma

2021

RJPT

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Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

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Formulation optimization and Evaluation of Transdermal patch of losartan potassium containing DMSO as permeation enhancer

Cited by 5 publications

References 0 publications

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

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Formulation and Evaluation of Transdermal patch of Methimazole

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